| Bioactivity | Amtolmetin guacil is an effective nonsteroidal anti-Inflammatory agent with pain-relieving effects. Amtolmetin guacil inhibits prostaglandin synthesis and cyclooxygenase (COX). Amtolmetin guacil can stimulate capsaicin receptors present on the gastrointestinal wall and also releases gastroprotective nitric oxide (NO). Amtolmetin guacil can be used to research knee osteoarthritis[1][2]. |
| Target | Prostaglandin receptor, COX, NO |
| Invitro | Amtolmetin guacil (100 μM; 0-60 min) converts to TMT (Tolmetin, HY-B1799) along with MED5 (1-methyl-5-p-methylbenzoyl-pyrrol-2-acetamido aceticacid) in rat fresh plasma and rat liver microsomal, rapidly converts to MED5 and MED5 methyl ester without yielding TMT in human fresh plasma and human liver microsomes[3]. |
| In Vivo | Animal Model: |
| Name | Amtolmetin guacil |
| CAS | 87344-06-7 |
| Formula | C24H24N2O5 |
| Molar Mass | 420.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Marcolongo, R., et al. A Meta-Analysis of the Tolerability of Amtolmetin Guacil, a Novel, Effective Nonsteroidal Anti-Inflammatory Drug, Compared with Established Agents. Clin. Drug Investig. 17, 89-96 (1999). [2]. Niccoli L, et al. Renal tolerability of three commonly employed non-steroidal anti-inflammatory drugs in elderly patients with osteoarthritis. Clin Exp Rheumatol. 2002 Mar-Apr;20(2):201-7. [3]. Hotha KK, et al. Species difference in the in vitro and in vivo metabolism of amtolmetin guacil. Arzneimittelforschung. 2010;60(11):667-74. |